The design and discovery of novel amide CCR5 antagonists

被引：18

作者：

Pryde, David C. ^{[1
]}

Corless, Martin ^{[1
]}

Fenwick, David R. ^{[1
]}

Mason, Helen J. ^{[1
]}

Stammen, Blanda C. ^{[1
]}

Stephenson, Peter T. ^{[1
]}

Ellis, David ^{[1
]}

Bachelor, David ^{[1
]}

Gordon, David ^{[1
]}

Barber, Christopher G. ^{[1
]}

Wood, Anthony ^{[1
]}

Middleton, Donald S. ^{[1
]}

Blakemore, David C. ^{[1
]}

Parsons, Gemma C. ^{[1
]}

Eastwood, Rachel ^{[1
]}

Platts, Michelle Y. ^{[1
]}

Statham, Keith ^{[1
]}

Paradowski, Kerry A. ^{[1
]}

Burt, Catherine ^{[1
]}

Klute, Wolfgang ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Dept Chem, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 04期

关键词：

CCR5; Antagonist; Chemokine; HIV; AIDS; Antiviral; SMALL-MOLECULE INHIBITOR; CHEMOKINE RECEPTOR CCR5; HIV-1; INFECTION; BIOLOGICAL EVALUATION; BINDING POCKET; POTENT; SCH-351125; ENTRY; UK-427,857; MARAVIROC;

D O I：

10.1016/j.bmcl.2009.01.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1084 / 1088

页数：5